Exenatide

What is Exenatide?

• Exenatide (Byetta and Bydureon) is a glucagon-like peptide-1 (GLP-1) receptor agonist which is used in combination with diet and exercise in the therapy of type 2 diabetes, either alone or in combination with other antidiabetic agents.
• Exenatide (Byetta) is used along with diet and exercise to treat type 2 diabetes in adults.
• Exenatide (Bydureon and Bydureon BCISE) is used along with diet and exercise to treat type 2 diabetes in adults and children 10 years of age and older.

Exenatide

Exenatide sequence

What are the uses of this medicine?

• Exenatide (Bydureon and Bydureon BCISE) is an injectable prescription medicine that may improve blood sugar (glucose) in adults and children who are 10 years of age and older with type 2 diabetes mellitus and should be used along with diet and exercise.

Limitations of Use:

• Bydureon/Bydureon BCISE is not recommended as the first choice of medicine for treating diabetes.
• Bydureon/Bydureon BCISE is not for use in people with type 1 diabetes.
• Bydureon and Bydureon BCise are long-acting forms of the medicine in BYETTA (exenatide). Bydureon should not be used at the same time as BYETTA or Bydureon BCise.
• It is not known if Bydureon/Bydureon BCISE can be used in people who have had pancreatitis.
• It is not known if Bydureon/Bydureon BCISE is safe and effective for use in children younger than 10 years of age.

How does this medicine work?

• Exenatide (ex en' a tide) is a synthetic analogue of glucagon-like peptide-1 (GLP-1) that acts like the native gastrointestinal hormone (incretin) to increase insulin secretion.
• Exenatide, like GLP-1, increases insulin secretion by the pancreas and can improve glycemic control in patients with type 2 diabetes. Exenatide is a polypeptide initially extracted from salivary glands of the Gila monster and has close homology (53%) to human GLP-1, but is resistant to DPP-4 degradation and thus has a prolonged duration of activity.
• Exenatide (also known as exendin-4) must be given parenterally.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• have ever had a type of thyroid cancer called medullary thyroid carcinoma (MTC) or if you have an endocrine system condition called Multiple Endocrine Neoplasia syndrome type 2 (MEN 2).
• have had a severe allergic reaction to exenatide or any of the ingredients in Bydureon.
• have a history of low blood platelet count from using exenatide medicines (drug-induced thrombocytopenia).

What drug interactions can this medicine cause?

• Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Be sure to mention any of the following:

• acetaminophen (Tylenol)
• angiotensin-converting enzyme (ACE) inhibitors such as benazepril (Lotensin, in Lotrel), captopril, enalapril (Epaned, Vasotec, in Vaseretic), fosinopril, lisinopril (Prinivil, Qbrelis, Zestril, in Zestoretic), moexipril, perindopril (in Prestalia), quinapril (Accupril, in Accuretic, in Quinaretic), ramipril (Altace), and trandolapril
• diuretics ('water pills')
• aspirin and other nonsteroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen (Advil, Motrin) and naproxen (Aleve, Naprosyn)
• lovastatin (Altoprev)
• medications for high blood pressure
• insulin or other medications to treat diabetes such as sulfonylureas, such as glimepiride (Amaryl, in Duetact), glipizide (Glucotrol), glyburide (DiaBeta, Glynase), and tolbutamide
• warfarin (Jantoven)

• If you are taking oral contraceptives (birth control pills) or antibiotics, take them at least 1 hour before you use exenatide immediate-release solution injection.

Is this medicine FDA approved?

• Exenatide was approved for use in the United States in 2005, and current indications are for the management of glycemic control in adults with type 2 diabetes used in combination with diet and exercise, with or without other oral hypoglycemic agents.

How should this medicine be used?

Recommended dosage:

• Administer 2 mg by subcutaneous injection once every seven days (weekly), at any time of day and with or without meals.

Administration:

• Bydureon/Bydureon BCISE should be injected right away after you prepare your dose.
• Bydureon/Bydureon BCISE is injected under the skin (subcutaneously) of your stomach (abdomen), thigh, or upper arm. Do not inject Bydureon/Bydureon BCISE into a muscle (intramuscularly) or vein (intravenously).
• Use Bydureon/Bydureon BCISE 1 time each week on the same day each week at any time of the day.
• Bydureon may be taken with or without food.
• If you miss a dose of Bydureon/Bydureon BCISE, take the missed dose as soon as possible if there are at least 3 days (72 hours) until your next scheduled dose. If there are less than 3 days remaining, skip the missed dose and take your next dose on the regularly scheduled day. Do not take 2 doses of Bydureon within 3 days of each other.
• You may change the day of the week as long as your last dose was given 3 or more days before.
• Do not mix insulin and Bydureon/Bydureon BCISE together in the same injection.
• You may give an injection of Bydureon/Bydureon BCISE and insulin in the same body area (such as, your stomach area), but not right next to each other.
• Change (rotate) your injection site with each weekly injection. Do not use the same site for each injection.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Extended-release injectable suspension

This medicine is available in fallowing brand namesː

• Bydureon; Bydureon BCISE

What side effects can this medication cause?

The most common side effects of this medicine include:

• nausea, diarrhea, headache, vomiting, constipation, itching at the injection site, a small bump (nodule) at the injection site, indigestion

Bydureon/Bydureon BCISE may cause serious side effects, including:

• Possible thyroid tumors, including cancer
• pancreatitis
• hypoglycemia
• kidney problems
• stomach problems
• serious allergic reactions
• drug-induced thrombocytopenia
• injection-site reactions
• gallbladder problems

What special precautions should I follow?

• Acute Pancreatitis including fatal and non-fatal hemorrhagic or necrotizing pancreatitis has been reported. Discontinue promptly if pancreatitis is suspected. Do not restart if pancreatitis is confirmed. Consider other antidiabetic therapies if patient has history of pancreatitis.
• Bydureon is contraindicated in patients with a personal or family history of medullary thyroid carcinoma (MTC) or in patients with Multiple Endocrine Neoplasia syndrome type 2 (MEN 2). Counsel patients regarding the potential risk of MTC and the symptoms of thyroid tumors.
• Patients receiving Bydureon in combination with an insulin secretagogue (e.g., sulfonylurea) or insulin may have an increased risk of hypoglycemia, including severe hypoglycemia. Reduction in the dose of insulin secretagogue or insulin may be necessary.
• Bydureon may induce nausea and vomiting with transient hypovolemia and may worsen renal function. Postmarketing increased serum creatinine, renal impairment, worsened chronic renal failure and acute renal failure, sometimes requiring hemodialysis or kidney transplantation has been reported. Not recommended for use in patients with eGFR below 45 mL/min/1.73 m2.
• Exenatide has not been studied in patients with severe gastrointestinal disease, including gastroparesis. Not recommended in patients with severe gastrointestinal disease (e.g., gastroparesis).
• Patients may develop antibodies to exenatide following treatment with Bydureon. If there is worsening glycemic control or failure to achieve target glycemic control, consider alternative antidiabetic therapy.
• There have been postmarketing reports of serious hypersensitivity reactions (e.g., anaphylaxis and angioedema) in patients treated with exenatide. In such cases, patients are to discontinue Bydureon and promptly seek medical advice.
• Serious bleeding, which may be fatal, from drug-induced immune-mediated thrombocytopenia has been reported in the postmarketing setting with exenatide use.
• Serious injection-site reactions with or without subcutaneous nodules have been reported.
• Acute events of gallbladder disease, such as cholelithiasis or cholecystitis, have been reported in GLP-1 receptor agonist. If cholelithiasis or cholecystitis are suspected, gallbladder studies are indicated.

What to do in case of emergency/overdose?

Symptoms of overdose may include:

• severe nausea, severe vomiting, and rapidly declining blood glucose concentrations, including severe hypoglycemia requiring parenteral glucose administration

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• In the event of overdose, appropriate supportive treatment should be initiated according to the patient's clinical signs and symptoms.

Can this medicine be used in pregnancy?

• Limited data with exenatide, the active ingredient in Bydureon, in pregnant women are not sufficient to determine a drug-associated risk for major birth defects or miscarriage.
• Bydureon should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Can this medicine be used in children?

• The safety and effectiveness of Bydureon as an adjunct to diet and exercise to improve glycemic control in type 2 diabetes mellitus have been established in pediatric patients aged 10 years and older.
• The safety and effectiveness of Bydureon have not been established in pediatric patients less than 10 years of age.

What are the active and inactive ingredients in this medicine?

• Active ingredient: exenatide.
• Inactive ingredients: polylactide-co-glycolide and sucrose.
• Contents of liquid (diluent):
• Inactive Ingredients: carboxymethylcellulose sodium, polysorbate 20, sodium phosphate monobasic monohydrate, sodium phosphate dibasic heptahydrate, sodium chloride, water for injection. Sodium hydroxide may be added during manufacture of Bydureon Pen for pH adjustment.

Who manufactures and distributes this medicine?

Bydureon and Bydureon, BCISE: Manufactured for:

• AstraZeneca Pharmaceuticals LP
• Wilmington, DE

By:

• Amylin Ohio LLC
• West Chester, OH

What should I know about storage and disposal of this medication?

Storage and Handling:

• Bydureon BCISE must be stored FLAT.
• Store the autoinjector in the original package. Protect from light. Do not use past the expiration date.
• Store Bydureon BCISE in the refrigerator at 36°F to 46°F (2°C to 8°C).
• Bydureon BCISE can be kept at room temperature not to exceed 86°F (30°C) for no more than a total of 4 weeks, if needed.
• Discard Bydureon BCISE after use in a puncture-resistant container.

• Store Bydureon in the refrigerator at 36°F to 46°F (2°C to 8°C).
• Do not freeze Bydureon. Do not use Bydureon if it has been frozen. Protect from light. Do not use past the expiration date.
• Bydureon can be kept at room temperature not to exceed 77°F (25°C) [see USP Controlled Room Temperature] for no more than a total of 4 weeks, if needed.
• Bydureon must be administered immediately after the exenatide powder is suspended in the diluent.

Antidiabetics

•  Alpha-Glucosidase Inhibitors
  • Acarbose
  • Miglitol
• Incretin-Based Drugs
  • Dipeptidyl Peptidase-4 (DPP-4) Inhibitors
    • Alogliptin
    • Linagliptin
    • Saxagliptin
    • Sitagliptin
  • Glucagon-Like Peptide-1 (GLP-1) Analogues
    • Albiglutide
    • Dulaglutide
    • Exenatide
    • Liraglutide
    • Lixisenatide
•  Insulin
• Metformin
• Metiglinide Analogues
  • Nateglinide
  • Repaglinide
• Pramlintide
• Sodium Glucose Cotransporter-2 (SGLT-2) Inhibitors
  • Canagliflozin
  • Dapagliflozin
  • Empagliflozin
• Sulfonylureas
  • First Generation Sulfonylureas
    • Acetohexamide
    • Chlorpropamide
    • Tolazamide
    • Tolbutamide
  • Second Generation Sulfonylureas
    • Gliclazide
    • Glimepiride
    • Glipizide
    • Glyburide (Glibenclamide)
• Thiazolidinediones
  • Pioglitazone
  • Rosiglitazone
  • Troglitazone

• Dailymed label info on Exenatide
• FDA Exenatide

Exenatide Resources
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